Clinical pharmacology of etintidine in patients with duodenal ulcer.

Abstract

The gastric antisecretory activity of etintidine, a new histamine H2-receptor antagonist, was evaluated in 5 patients with quiescent duodenal ulcer disease. Meal-stimulated acid secretion was measured after 100 and 300 mg oral doses of etintidine, 100 and 300 mg oral doses of cimetidine, and placebo. Reductions from placebo in four-hour gastric acid secretion were 49, 65, 80, and 94%, with 100 mg cimetidine, 100 mg etintidine, 300 mg cimetidine, and 300 mg etintidine, respectively. Drug concentrations in plasma were determined by HPLC. The pharmacokinetics of the 2 drugs were similar. We analyzed sigmoid-shaped concentration-response curves to both agents; the concentrations causing 50% inhibition of meal-stimulated gastric acid secretion were 0.44 +/- 0.04 and 0.15 +/- 0.04 micrograms/ml for cimetidine and etintidine, respectively. However, characteristics of these curves were such that the potency difference diminished at higher concentrations.

• Authors: D C Brater, W M Meyers Jr, K A Dandekar, K A Pittman, W Peterson
• Journal: European journal of clinical pharmacology (Eur J Clin Pharmacol) Vol. 23 Issue 6 Pg. 495-500 ( 1982) ISSN: 0031-6970 [Print] Germany
• PMID: 6130952 (Publication Type: Clinical Trial, Controlled Clinical Trial, Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, Non-P.H.S., Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Gastrins
• Histamine H2 Antagonists
• Imidazoles
• Cimetidine
• etintidine

Topics

• Cimetidine (blood, therapeutic use)
• Duodenal Ulcer (drug therapy)
• Female
• Gastric Acid (metabolism)
• Gastric Acidity Determination
• Gastrins (blood)
• Histamine H2 Antagonists (metabolism, therapeutic use)
• Humans
• Imidazoles (blood, therapeutic use)
• Kinetics
• Male
• Middle Aged